Transdermal compositions

Abstract

The present invention is directed to transdermal compositions and the uses thereof. These compositions include at least one of the following components: a C 1 -C 6 dialkyl, C 12 -C 30 dialkyl quaternary ammonium salt, a C 12 -C 30 fatty acid, a nitrogenous organic base, C 12 -C 30 fatty alcohol, monoglyceride or the reaction products thereof.

1. A composition comprising an antimicrobial effective amount of povidone iodine and tertiary amide of the formula: 
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof wherein R 4  is a fatty group of 11-29 carbon atoms;
 R 5  and R 6  are independently lower alkyl, aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms or R 7 ; 
 R 7  is
   R 1 —Ar—O—R 2 —O—R 3 —;
 
 
 R 2  and R 3  are independently lower alkylene groups containing 1-6 carbon atoms, 
 R 1  is a lower alkyl, and 
 Ar is aryl. 
 
     
     
       2. The composition of  claim 1  wherein R 4  is a fatty group containing 15-21 carbon atoms. 
     
     
       3. The composition of  claim 1  wherein R 5  is aryl or aryl lower alkyl; and R 6  is
   R 1 —Ar—O—R 2 —O—R 3 —;
 
 R 2  and R 3  are independently alkylene containing 1-3 carbon atoms; and 
 Ar is aryl. 
 
     
     
       4. The composition according to  claim 3  wherein Ar is phenyl. 
     
     
       5. The composition according to  claim 4  wherein R 5  is aryl lower alkyl. 
     
     
       6. The composition according to  claim 5  wherein R 5  is benzyl. 
     
     
       7. The composition according to  claim 5  wherein R 4  is saturated, 
     
     
       8. The composition according to  claim 5  wherein R 4  is unsaturated. 
     
     
       9. The composition according to  claim 8  wherein R 4  contains 1-8 carbon-carbon double bonds. 
     
     
       10. The composition according to  claim 1  wherein the tertiary amide is distearyl stearamide, distearyl linoleamide, benzethonium linoleamide or benzethonium stearamide. 
     
     
       11. The composition according to  claim 1  wherein the povidone iodine is present in an amount ranging from about 3% to about 15% by weight of the composition. 
     
     
       12. The composition according to  claim 11  wherein the povidone-iodine is present in an amount ranging from about 5% to about 10% by weight of the composition. 
     
     
       13. The composition according to  claim 12  wherein the povidone iodine is present in an amount ranging from about 6% to about 8% by weight of the composition. 
     
     
       14. The composition according to  claim 1  in the form of a cream. 
     
     
       15. A composition comprising an anti-microbial effective amount of povidone-iodine and a tertiary amide of the formula: 
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof wherein
 R 4  is a fatty group of 11-29 carbon atoms; 
 R 5  and R 6  are independently aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms containing one to eight carbon-carbon double bonds or R 7 ; 
 R 7  is
   R 1 —Ar—O—R 2 —O—R 3 —;
 
 
 R 2  and R 3  are independently lower alkyl alkylene groups containing 1-6 carbon atoms; 
 R 1  is an alkyl group containing 1-15 carbon atoms; and 
 Ar is aryl. 
 
     
     
       16. The composition according to  claim 15  when R 4  is a fatty group containing 15-21 carbon atoms. 
     
     
       17. The composition according to  claim 15  in the form of a cream. 
     
     
       18. A composition comprising an anti-microbial effective amount of povidone-iodine and a tertiary amide hydrate formed from the process comprising heating a mixture of water, a quaternary surfactant, a fatty acid and an alkanolamine at a temperature greater than the melting point of said acid and less than 100° C. for sufficient time and under conditions effective to form a tertiary amide, cooling said tertiary amide to ambient temperature for sufficient time and under effective conditions for the pH of the water to stabilize and for said tertiary amide hydrate to form. 
     
     
       19. The composition according to  claim 18  wherein the tertiary amide hydrate wherein the alkanolamine is triethanolamine, trimethanolamine, tris (hydroxyethyl) aminomethane, or tris (hydroxyethyl methyl) aminoethane. 
     
     
       20. A composition comprising an anti-microbial effective amount of povidine-iodine and a therapeutically effective amount of an amide hydrate of a tertiary amide, where the tertiary amide has the formula: 
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof wherein
 R 4  is a fatty group of 11-29 carbon atoms; 
 R 5  and R 6  are independently lower alkyl, aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms or R 7 ; 
 R 7  is
   R 1 —Ar—O—R 2 —O—R 3 —;
 
 
 R 2  and R 3  are independently alkylene groups containing 1-6 carbon atoms; 
 R 1  is an alkyl group containing 1-15 carbon atoms; and 
 Ar is aryl. 
 
     
     
       21. The composition according to  claim 20  wherein R 4  is a fatty group containing 15-21 carbon atoms. 
     
     
       22. The composition according to  claim 20  wherein R 5  is aryl or aryl lower alkyl; and
 R 6  is
   R 1 —Ar—O—R 2 —O—R 3 —
 
 
 R 2  and R 3  are independently alkylene containing 1-3 carbon atoms; and 
 Ar is aryl. 
 
     
     
       23. The composition according to  claim 22  wherein Ar is phenyl. 
     
     
       24. The composition according to  claim 23  wherein R 5  is lower aryl lower alkyl. 
     
     
       25. The composition according to  claim 24  wherein R 5  is benzyl. 
     
     
       26. The composition according to  claim 25  wherein R 4  is saturated. 
     
     
       27. The composition according to  claim 25  wherein R 4  is unsaturated. 
     
     
       28. The composition according to  claim 27  wherein R 4  contains 1-8 carbon-carbon double bonds. 
     
     
       29. The composition according to  claim 20  wherein the amide hydrate is the amide hydrate of a tertiary amide selected from the group consisting of distearyl stearamide, distearyl linoleamide, benzethonium linoleamide and benzethonium stearamide. 
     
     
       30. The composition according to  claim 15  or  20  wherein the povidone iodine is present in an amount ranging from about 3% to about 15% by weight of the composition. 
     
     
       31. The composition according to  claim 30  wherein the povidone-iodine is present in an amount ranging from about 5% to about 10% by weight of the composition. 
     
     
       32. The composition according to  claim 31  wherein the povidone iodine is present in an amount ranging from about 6% to about 8% by weight of the composition. 
     
     
       33. The composition according to  claim 20  in the form of a cream.